头孢克肟双层渗透泵控释片的研制与评价

R. Tyagi, P. Sharma, D. Gupta
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引用次数: 0

摘要

背景:本研究旨在研制头孢克肟渗透片,并对其进行优化和评价。它改善了场地规格,并通过该给药系统提供每天一次的药物控制释放。头孢克肟除可溶性外,在可溶性限制中占有重要地位。通过制备渗透片剂可提高药物的生物利用度。方法:以氯化钠、PVP K30、微晶纤维素等不同比例的原料配制成控孔渗透片(CP1 - CP9)。芯片的涂层由醋酸纤维素peg400按统计比例完成。结果:根据硬度、直径、脆度、重量变化、含量均匀度、体外释放度等评价指标,CP9制剂效果较好。释药率>95%。优化后的CP9批与零级释药动力学模型相关度最高,为0.992。结论:研制了一种基于渗透技术的头孢克肟控释制剂。该制剂的释放与释放介质的pH和搅拌强度无关;该制剂符合零级动力学,表明释放与药物负荷无关。药物释放量与初始孔隙水平成正比,与膜重成反比。释放与释放介质的渗透压呈负相关,证实了渗透泵是释放的主要机制。
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FORMULATION AND EVALUATION OF DUAL-LAYERED OSMOTIC PUMP CONTROLLED-RELEASE TABLETS OF CEFIXIME
Background: This study aims to formulate, optimize and evaluate the osmotic tablet of cefixime. It improves the site specification and provides the controlled release of drug once – a – day through this drug delivery system. Cefixime assumes a significant part in dissolvability restricts other than dissolvable sort. It might increase the bioavailability of drugs by the preparation of the osmotic tablet. Method: The forming core tablet does a formulation of Controlled Porosity Osmotic Tablets (CP1 – CP9) using an ingredient like sodium chloride, PVP K30, Microcrystalline cellulose various ratios. The coating of the core tablet is done by Cellulose Acetate, PEG 400, with statistical ratios. Result: On depending upon the various evaluation parameters like hardness, diameter, friability, weight variation, content uniformity, In vitro release, CP9 formulation gave better consequence. The percentage of drug release is >95%. The optimized CP9 batch showed a maximum correlation of 0.992 with a zero-order drug release kinetic model. Conclusion: A controlled release formulation of cefixime based on osmotic technology, were developed. The release from the developed formulation was independent of pH and agitational intensity of the release media; the formulation fitted well into zero-order kinetics, indicating the release to be drug load independent. Drug release was directly proportional to the initial pore level but inversely related to the membrane weight. The release was inversely associated with the release media's osmotic pressure, confirming osmotic pumping as the central mechanism of release.
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